Title: Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-Noxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs.
Authors: Ancizu, Saioa; Moreno, Elsa; Torres, Enrique; Burguete, Asunción; Pérez-Silanes, Silvia; Benítez, Diego; Villar, Raquel; Solano, Beatriz; Marín, Adoración; Aldana, Ignacio; Cerecetto, Hugo; González, Mercedes; Monge, Antonio
Abstract: Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis (TB). Besides TB, Chagas disease, affects approximately 20 million people. Quinoxalines display great activities against TB and Chagas. Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi. Carboxylic acid quinoxaline 1,4-di-N-oxides (CAQDOs) 5 and 17 showed MIC values on the same order as the reference antituberculosis drug, rifampicin. Meanwhile, CAQDOs 12 and 22 presented IC50 values in the same order as the anti-chagasic drug, nifurtimox.
Subjects: CARBOXYLIC acids; TUBERCULOSIS treatment; CHAGAS' disease treatment; QUINOXALINES; RIFAMPIN; MYCOBACTERIUM tuberculosis; TRYPANOSOMA cruzi; MYCOBACTERIAL diseases; THERAPEUTICS
Publication: Molecules, 2009, Vol 14, Issue 6, p2256
ISSN: 1420-3049
Publication type: Academic Journal
DOI: 10.3390/molecules14062256

Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-Noxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs.

Ancizu, Saioa; Moreno, Elsa; Torres, Enrique; Burguete, Asunción; Pérez-Silanes, Silvia; Benítez, Diego; Villar, Raquel; Solano, Beatriz; Marín, Adoración; Aldana, Ignacio; Cerecetto, Hugo; González, Mercedes; Monge, Antonio